产品
编 号：F751660
分子式：C28H27N5O
分子量：449.55
分子式：C28H27N5O
分子量：449.55
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
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询价
结构图
CAS No: 2375554-02-0
产品详情
生物活性：
Senexin C is a selective and orally active CDK8/19 inhibitor. Senexin C shows a strong tumor-enrichment pharmacokinetic (PK) profile and tumor-pharmacodynamic (PD) marker responses. Senexin C inhibits the growth of MV4-11 leukemia cells with good tolerability.
体内研究：
Senexin C (2.5 mg/kg, i.v.; 100 mg/kg, p.o.) shows good oral bioavailability.Senexin C (40 mg/kg; p.o.; twice daily for 4 weeks) suppresses the systemic growth of MV4-11 AML with good tolerability.Pharmacokinetic Parameters of Senexin C in eight-week-old female Balb/c mice.parametersiv (2.5 mg/kg)po (100 mg/kg)
plasmatumorplasmatumor
C0 (μg/mL)503
Kel (h-1)0.930.060.20.1
T1/2 (h)0.7512.13.537.27
Tmax (h)0.581212
Cmax (ng/mL or ng/g)4881445728
AUC0-24 h (ng x h/ml or ng x h/g)3316408218288,600
F%16.5%34.6%
Eight-week-old female Balb/c mice ( CT26 tumor mode), 2.5 mg/kg, i.v.(2.5 mg/mL Senexin C solution in 5% dextrose); 100 mg/kg, p.o.(10 mg/mL Senexin C solution in 30% propylene glycol/70% PEG-400 vehicle).Animal Model:eight-week-old female Balb/c mice ( CT26 tumor mode)
Dosage:2.5 mg/kg (10 mL/kg of 2.5 mg/mL Senexin C solution in 5% dextrose), 100 mg/kg (10 mL/kg of 10 mg/mL Senexin C solution in 30% propylene glycol/70% PEG-400 vehicle)
Administration:2.5 mg/kg, i.v.; 100 mg/kg, p.o.
Result:Showed good oral bioavailability.
Animal Model:eight-week-old female NSG mice ( AML model)
Dosage:40 mg/kg
Administration:p.o.; twice daily, 4 weeks
Result:Suppressed the systemic growth of MV4-11 AML with good tolerability.
体外研究：
Senexin C (compound 20a) exhibits potent CDK8/19 inhibitory activity with high selectivity (IC50s of 56 and 108 nM for 293-NFκB-Luc and MV4-11-Luc cells, respectively).Senexin C (2 μM) shows potency in different kinase assays (IC50= 3.6 nM for CD8/CycC, Kd=1.4 nM for CD8/CycC, Kd=2.9 nM for CDK19/CycC).Senexin C (1 μM, 3 h) shows inhibition on CDK8/19 dependent cellular gene expression.
Senexin C is a selective and orally active CDK8/19 inhibitor. Senexin C shows a strong tumor-enrichment pharmacokinetic (PK) profile and tumor-pharmacodynamic (PD) marker responses. Senexin C inhibits the growth of MV4-11 leukemia cells with good tolerability.
体内研究：
Senexin C (2.5 mg/kg, i.v.; 100 mg/kg, p.o.) shows good oral bioavailability.Senexin C (40 mg/kg; p.o.; twice daily for 4 weeks) suppresses the systemic growth of MV4-11 AML with good tolerability.Pharmacokinetic Parameters of Senexin C in eight-week-old female Balb/c mice.parametersiv (2.5 mg/kg)po (100 mg/kg)
plasmatumorplasmatumor
C0 (μg/mL)503
Kel (h-1)0.930.060.20.1
T1/2 (h)0.7512.13.537.27
Tmax (h)0.581212
Cmax (ng/mL or ng/g)4881445728
AUC0-24 h (ng x h/ml or ng x h/g)3316408218288,600
F%16.5%34.6%
Eight-week-old female Balb/c mice ( CT26 tumor mode), 2.5 mg/kg, i.v.(2.5 mg/mL Senexin C solution in 5% dextrose); 100 mg/kg, p.o.(10 mg/mL Senexin C solution in 30% propylene glycol/70% PEG-400 vehicle).Animal Model:eight-week-old female Balb/c mice ( CT26 tumor mode)
Dosage:2.5 mg/kg (10 mL/kg of 2.5 mg/mL Senexin C solution in 5% dextrose), 100 mg/kg (10 mL/kg of 10 mg/mL Senexin C solution in 30% propylene glycol/70% PEG-400 vehicle)
Administration:2.5 mg/kg, i.v.; 100 mg/kg, p.o.
Result:Showed good oral bioavailability.
Animal Model:eight-week-old female NSG mice ( AML model)
Dosage:40 mg/kg
Administration:p.o.; twice daily, 4 weeks
Result:Suppressed the systemic growth of MV4-11 AML with good tolerability.
体外研究：
Senexin C (compound 20a) exhibits potent CDK8/19 inhibitory activity with high selectivity (IC50s of 56 and 108 nM for 293-NFκB-Luc and MV4-11-Luc cells, respectively).Senexin C (2 μM) shows potency in different kinase assays (IC50= 3.6 nM for CD8/CycC, Kd=1.4 nM for CD8/CycC, Kd=2.9 nM for CDK19/CycC).Senexin C (1 μM, 3 h) shows inhibition on CDK8/19 dependent cellular gene expression.
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